Cited by 395Angiogenesis and VEGF in CancerCancer Mechanisms and TherapyProtease and Inhibitor Mechanisms

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Inhibition of Tumor Cell Growth, Invasion, and Metastasis by EXEL-2880 (XL880, GSK1363089), a Novel Inhibitor of HGF and VEGF Receptor Tyrosine Kinases

Qian, Fawn, Engst, Stefan, Yamaguchi, Kyoko, Yu, Peiwen, Won, Kwang-Ai, Mock, Lillian, Lou, Tracy, Tan, Jenny, Li, Connie, Tam, Danny, Lougheed, Julie, Yakes, F. Michael, Bentzien, Frauke, Xu, Wei, Zaks, Tal, Wooster, Richard, Greshock, Joel, Joly, Alison H.·2009·Cancer Research

DOI 10.1158/0008-5472.can-08-4889

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Abstract

The Met receptor tyrosine kinase and its ligand, hepatocyte growth factor (HGF), are overexpressed and/or activated in a wide variety of human malignancies. Vascular endothelial growth factor (VEGF) receptors are expressed on the surface of vascular endothelial cells and cooperate with Met to induce tumor invasion and vascularization. EXEL-2880 (XL880, GSK1363089) is a small-molecule kinase inhibitor that targets members of the HGF and VEGF receptor tyrosine kinase families, with additional inhibitory activity toward KIT, Flt-3, platelet-derived growth factor receptor β, and Tie-2. Binding of EXEL-2880 to Met and VEGF receptor 2 (KDR) is characterized by a very slow off-rate, consistent with X-ray crystallographic data showing that the inhibitor is deeply bound in the Met kinase active site cleft. EXEL-2880 inhibits cellular HGF-induced Met phosphorylation and VEGF-induced extracellular signal-regulated kinase phosphorylation and prevents both HGF-induced responses of tumor cells and HGF/VEGF-induced responses of endothelial cells. In addition, EXEL-2880 prevents anchorage-independent proliferation of tumor cells under both normoxic and hypoxic conditions. In vivo, these effects produce significant dose-dependent inhibition of tumor burden in an experimental model of lung metastasis. Collectively, these data indicate that EXEL-2880 may prevent tumor growth through a direct effect on tumor cell proliferation and by inhibition of invasion and angiogenesis mediated by HGF and VEGF receptors. [Cancer Res 2009;69(20):8009–16]

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Authors: Qian, F., Engst, S., Yamaguchi, K., Yu, P., Won, K.-A., Mock, L., Lou, T., Tan, J., Li, C., Tam, D., Lougheed, J., Yakes, F. M., Bentzien, F., Xu, W., Zaks, T., Wooster, R., Greshock, J., & Joly, A. H.
Affiliations: Exelixis (United States) (US)
1Exelixis, Inc., South San Francisco, California and
GlaxoSmithKline (United States) (US)
ORCID: Yu, Peiwen
Lou, Tracy
Tan, Jenny
Li, Connie
Xu, Wei
Greshock, Joel
Venue: Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2009-10-14
Volume: 69
Issue: 20
Pages: 8009-8016
ISSN: 0008-5472 (ISSN-L)
1538-7445
DOI: 10.1158/0008-5472.can-08-4889
OpenAlex: W2130921495
Cited by: 350
References: 48
Citations by year: 2026: 11 · 2025: 9 · 2024: 18 · 2023: 24 · 2022: 14 · 2021: 25 · 2020: 20 · 2019: 12 · 2018: 13 · 2017: 26 · 2016: 17 · 2015: 31 · 2014: 20 · 2013: 44 · 2012: 27
FWCI: 8.87
Type: journal article
Language: en
Open access: closed
Locations: Cancer Research (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Angiogenesis and VEGF in Cancer
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Mechanisms and Therapy
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Protease and Inhibitor Mechanisms
Keywords: MET receptor tyrosine kinase, hepatocyte growth factor, tyrosine kinase inhibitors, tumor invasion, lung metastasis, angiogenesis, tumor cell proliferation, hypoxia, endothelial cells, KIT, FLT3, PDGFRβ, Tie2
MeSH terms: Anilides, Animals, Cell Adhesion, Cell Movement, Cells, Cultured, Endothelium, Vascular, Enzyme-Linked Immunosorbent Assay, Female, Fibroblasts, Humans, Lung Neoplasms, Mice, Inbred BALB C, Mice, Nude, Neoplasm Invasiveness, Neoplasms, Experimental, Neovascularization, Pathologic, Phosphorylation, Quinolines, Umbilical Veins, Blotting, Western, Apoptosis, Hepatocyte Growth Factor, Proto-Oncogene Proteins c-met, Dermis, Receptors, Vascular Endothelial Growth Factor, Protein Kinase Inhibitors, Cell Proliferation, Mice

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Inhibition of Tumor Cell Growth, Invasion, and Metastasis by EXEL-2880 (XL880, GSK1363089), a Novel Inhibitor of HGF and VEGF Receptor Tyrosine Kinases

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